CN103948933A - Resveratrol clathrate and preparation method of resveratrol clathrate preparations - Google Patents
Resveratrol clathrate and preparation method of resveratrol clathrate preparations Download PDFInfo
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- CN103948933A CN103948933A CN201410077746.2A CN201410077746A CN103948933A CN 103948933 A CN103948933 A CN 103948933A CN 201410077746 A CN201410077746 A CN 201410077746A CN 103948933 A CN103948933 A CN 103948933A
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- resveratrol
- clathrate
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Abstract
The invention belongs to the technical field of medicines, and relates to a resveratrol clathrate and a preparation method of resveratrol clathrate preparations, and the method mainly includes the following content: (1) selecting a suitable solvent to dissolve resveratrol; (2) using a modern preparation technology, comprising a saturated water solution method, a grinding method, a freeze drying method, an ultrasonic method, a spray drying method and the like, and a new clathrate material, comprising cyclodextrin or its derivatives such as beta cyclodextrin, hydroxypropyl beta cyclodextrin, alpha cyclodextrin, gamma cyclodextrin, glucosyl beta cyclodextrin and the like, to prepare the resveratrol clathrate; (3) using experiments to optimize a best mass ratio of resveratrol to clathrate material molecule; and (4) preparing the resveratrol clathrate into tablets, capsules, oral liquids and other preparations. By preparation of the resveratrol clathrate and the resveratrol clathrate preparations, the problem of poor water solubility and instability and low bioavailability can be solved.
Description
Technical field
The invention belongs to medical technical field, be specifically related to the preparation method of resveratrol cyclodextrin clathrate and preparation thereof.
Background technology
Resveratrol belongs to polyphenol compound, is called again resvertrol, is mainly derived from the plants such as Fructus Vitis viniferae (red wine), Rhizoma Polygoni Cuspidati, Semen arachidis hypogaeae, Fructus Mori.Resveratrol is a kind of multiple bioactive natural product that has: being not only the chemopreventive agent of tumor, is also to reduce platelet aggregation, the chemopreventive agent of prevention and treatment atherosclerosis, cardiovascular and cerebrovascular disease.Chinese scholars not only has preventive and therapeutic action to cardiovascular disease by studies confirm that resveratrol, and cancer is had to preventive effect equally, especially hormone-dependent tumor is had to obvious preventive effect; In addition resveratrol also has preventive effect to osteoporosis, acne and senile dementia, has antiviral and immunoregulatory pharmacological action.But resveratrol is insoluble in water (dissolubility is 0.03 g/L in water), oral absorption is poor, bioavailability is lower, under ultra-vioket radiation, easily there is isomerization, be difficult to reach the therapeutic effect of expection, therefore utilize new agent technology that it is first made to clathrate, further making various preparations, will greatly improve its stability and bioavailability.
Summary of the invention
The present invention uses modern preparation technique, adopt novel enclose rings of material dextrin or derivatives thereof that its enclose is formed to resveratrol cyclodextrin clathrate, stability and the bioavailability of resveratrol have greatly been improved, and make various dosage forms, enrich the preparation variety of this class medicine, expanded the application prospect of resveratrol.
Technical scheme of the present invention is as follows:
The present invention selects cyclodextrin or derivatives thereof (beta-schardinger dextrin-, HP-β-CD) as enclose material, resveratrol to be made to cyclodextrin clathrate;
Resveratrol cyclodextrin clathrate of the present invention, the mass ratio 1-5:1 of cyclodextrin used and resveratrol, the mass ratio 1-10:1-2 of HP-β-CD and resveratrol;
The preparation of resveratrol clathrate of the present invention: resveratrol, with after suitable organic solvent dissolution, carries out enclose.Solvent used can be ether, chloroform, methanol, ethanol, acetone, ethyl acetate;
The made resveratrol cyclodextrin clathrate of the present invention can be prepared into tablet, capsule, oral liquid;
The invention solves resveratrol water solublity problem, stability and bioavailability improve greatly.
The specific embodiment
Embodiment 1
The preparation of resveratrol clathrate: get 10g beta-schardinger dextrin-and make saturated aqueous solution, magnetic agitation, take resveratrol 5g, after a small amount of anhydrous alcohol solution, slowly splash in above-mentioned beta-schardinger dextrin-saturated aqueous solution, be stirred to the fixed time, after 4 ℃ of cold preservation 24h, decompress filter, a small amount of absolute ethanol washing filter cake, filter cake is dried to constant weight under vacuum, obtains clathrate powder.
Embodiment 2
Supercritical ultrasonics technology is prepared resveratrol clathrate: get 30g beta-schardinger dextrin-and make saturated aqueous solution, add the alcoholic solution of 10g resveratrol, after mixing, by ultrasonic Treatment, will separate out precipitation through solvent wash, dry, obtain clathrate powder.
Embodiment 3
The preparation of resveratrol hydroxypropyl-beta-cyclodextrin inclusion: get HP-β-CD 10g, with after water dissolution, the alcoholic solution of 10 g resveratrols is added, stir, dry, gained solution decompression is dry, obtains white powder hydroxypropyl-beta-cyclodextrin inclusion.
Embodiment 4
The tablet preparation of clathrate: by resveratrol beta-schardinger dextrin-9g, amylum pregelatinisatum 3 g, magnesium stearate is appropriate, mixes gained powder directly compressible.
Embodiment 5
Clathrate hard capsule: after embodiment 4 prescriptions are mixed, gained powder can directly fill hard capsule.
Embodiment 6
Oral resveratrol liquid preparation: by the hydroxypropyl-beta-cyclodextrin inclusion 10g of resveratrol, glucide is dissolved in 90mL water for injection in right amount, and with water for injection standardize solution 100mL processed, mixes, and obtains.
Claims (4)
1. resveratrol cyclodextrin clathrate and a preparation thereof, is characterized in that: utilize cyclodextrin and derivant thereof to improve dissolubility and the stability of resveratrol in water, and make oral formulations.
2. resveratrol clathrate and the preparation thereof of claim 1, wherein cyclodextrin is that beta-schardinger dextrin-, hydroxy propyl-Beta-ring are stuck with paste.
3. resveratrol clathrate according to claim 1 and preparation thereof, is characterized in that: the mass ratio 1-5:1 of cyclodextrin used and resveratrol, the mass ratio 1:10-1:2 of HP-β-CD and resveratrol.
4. resveratrol clathrate according to claim 1 and preparation thereof, is characterized in that: said oral formulations comprises tablet, oral liquid, capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201410077746.2A CN103948933A (en) | 2014-03-05 | 2014-03-05 | Resveratrol clathrate and preparation method of resveratrol clathrate preparations |
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| CN201410077746.2A CN103948933A (en) | 2014-03-05 | 2014-03-05 | Resveratrol clathrate and preparation method of resveratrol clathrate preparations |
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| CN103948933A true CN103948933A (en) | 2014-07-30 |
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| CN201410077746.2A Pending CN103948933A (en) | 2014-03-05 | 2014-03-05 | Resveratrol clathrate and preparation method of resveratrol clathrate preparations |
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105903033A (en) * | 2016-06-21 | 2016-08-31 | 重庆医科大学 | Resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and preparing method thereof |
| CN107280988A (en) * | 2017-07-03 | 2017-10-24 | 李剑峰 | Resveratrol cyclodextrin inclusion compound, oligopeptide facial mask liquid and preparation method thereof |
| CN107281033A (en) * | 2017-07-03 | 2017-10-24 | 李剑峰 | Sleep mask of acne scar acne print and its preparation method and application can be repaired |
| CN107375047A (en) * | 2017-07-03 | 2017-11-24 | 李剑峰 | Resveratrol cyclodextrin inclusion compound gel and its preparation method and application |
| EP3603415A1 (en) * | 2018-07-30 | 2020-02-05 | Universite D'Avignon et Des Pays Du Vaucluse | Method for extracting phenolic compounds |
| CN111265496A (en) * | 2018-12-04 | 2020-06-12 | 高雄医学大学 | Anti-haze compositions |
| CN111849021A (en) * | 2019-04-28 | 2020-10-30 | 南京理工大学 | Preparation method of polytetrafluoroethylene/hydroxypropyl-beta-cyclodextrin-resveratrol antioxidant film |
| CN114304633A (en) * | 2022-01-04 | 2022-04-12 | 中南大学 | Resveratrol-piperine compound microcapsule as well as preparation method and application thereof |
| CN118021996A (en) * | 2024-01-16 | 2024-05-14 | 华南理工大学 | Antibacterial inclusion material and preparation method and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1500479A (en) * | 2002-11-15 | 2004-06-02 | 董英杰 | resveratrol , piceid and its derivative and its preparation |
| CN102429888A (en) * | 2011-12-30 | 2012-05-02 | 湖南农业大学 | Water-soluble resveratrol effervescent tablet and preparation method thereof |
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2014
- 2014-03-05 CN CN201410077746.2A patent/CN103948933A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1500479A (en) * | 2002-11-15 | 2004-06-02 | 董英杰 | resveratrol , piceid and its derivative and its preparation |
| CN102429888A (en) * | 2011-12-30 | 2012-05-02 | 湖南农业大学 | Water-soluble resveratrol effervescent tablet and preparation method thereof |
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105903033A (en) * | 2016-06-21 | 2016-08-31 | 重庆医科大学 | Resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and preparing method thereof |
| CN107280988A (en) * | 2017-07-03 | 2017-10-24 | 李剑峰 | Resveratrol cyclodextrin inclusion compound, oligopeptide facial mask liquid and preparation method thereof |
| CN107281033A (en) * | 2017-07-03 | 2017-10-24 | 李剑峰 | Sleep mask of acne scar acne print and its preparation method and application can be repaired |
| CN107375047A (en) * | 2017-07-03 | 2017-11-24 | 李剑峰 | Resveratrol cyclodextrin inclusion compound gel and its preparation method and application |
| EP3603415A1 (en) * | 2018-07-30 | 2020-02-05 | Universite D'Avignon et Des Pays Du Vaucluse | Method for extracting phenolic compounds |
| WO2020025550A1 (en) * | 2018-07-30 | 2020-02-06 | Universite D'avignon Et Des Pays De Vaucluse | Method for extraction of phenol compounds |
| CN111265496A (en) * | 2018-12-04 | 2020-06-12 | 高雄医学大学 | Anti-haze compositions |
| CN111849021A (en) * | 2019-04-28 | 2020-10-30 | 南京理工大学 | Preparation method of polytetrafluoroethylene/hydroxypropyl-beta-cyclodextrin-resveratrol antioxidant film |
| CN114304633A (en) * | 2022-01-04 | 2022-04-12 | 中南大学 | Resveratrol-piperine compound microcapsule as well as preparation method and application thereof |
| CN118021996A (en) * | 2024-01-16 | 2024-05-14 | 华南理工大学 | Antibacterial inclusion material and preparation method and application thereof |
| CN118021996B (en) * | 2024-01-16 | 2024-07-30 | 华南理工大学 | Antibacterial inclusion material and preparation method and application thereof |
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Application publication date: 20140730 |
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